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Class 548/517 - Additional hetero ring, which is attached directly or indirectly to the five-membered hetero ring by nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein an additional hetero ring is attached
No. of patents: 727
Last issue date: 02/28/2012


1                      
NumberTitleIssue Date
8124790Preparation process useful in synthesis of atorvastatin
The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting...
02/28/2012
7943786Process for preparing amorphous (4R-cis)-6-[2-[3-phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]-dioxane-4-yl-acetic acid
The invention relates to a process of preparing amorphous (4R-cis)-6-[2-[3-phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]-dioxane-4-yl-acetic acid-tertiary butyl ester which is a useful pharmaceutical intermedi...
05/17/2011
77724053-alkyl-5- (4-alkyl-5-oxo-tetrahydrofutran-2-yl) pyrrolidin-2-one derivatives as intermediates in the synthesis of renin inhibitors
The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of ...
08/10/2010
7563910Heterocyclic cannabinoid receptor antagonists
The present invention relates to compounds of formula I and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB...
07/21/2009
RE40525Hepatitis C inhibitor tri-peptides
A racemate diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted wi...
09/30/2008
7429603C-fms kinase inhibitors
The invention is directed to compounds of Formulae I, II and III: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomer...
09/30/2008
7425575Spirocyclic 3-phenyl-3-substituted 4-ketolactams and 4-ketolactones
The present invention relates to novel phenyl-substituted 4-ketolactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y, Z and R3 are as defined above, ...
09/16/2008
7423061Substitute thiophenes and uses thereof
This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer. ...
09/09/2008
7417062Substituted arylamides
Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer. ...
08/26/2008
7414141Process and intermediate compounds useful in the preparation of statins, particularly atorvastatin
There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R1 represents a hydrogen or a hydrocarbyl group, R2 represents a hydrogen or substituent group, R3 represents a hydrogen or a hydr...
08/19/2008
7399773Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1-pyrrole-3-carboxylic acid and phenylamide
An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight ...
07/15/2008
7396851Heterocyclic and benzoheterocyclic polyamides structurally related to the natural antibiotic distamycin A for the treatment of β-thalassaemia
The invention relates to the use of structural analogues of distamycin having the general formula (I), (II), (III), (IV) or (V) or their pharmaceutically acceptable salts, for the preparation of a medicament for the therapeutic treatment of β-thalassaemia. ...
07/08/2008
7388007Gamma-lactams as beta-secretase inhibitors
There is provided a series of novel substituted gamma-lactams of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5 and R6
06/17/2008
73817413-amino-2-phenylpyrrolidine derivatives
3-amino-2-phenylpyrrolidine compounds useful as NK-1 antagonists, with pharmaceutical compositions and methods of treatment comprising same, are disclosed. ...
06/03/2008
7378436Compounds
A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl ...
05/27/2008
7371855Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1-pyrrole-3-carboxylic acid phenylamide
An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight ...
05/13/2008
7365092Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they ac...
04/29/2008
7361755Transition-metal-catalyzed process for the conversion of alkenes to sterically hindered substituted n-alkoxyamines
This invention pertains to a novel process for preparing sterically hindered N-substituted alkyloxyamines from alkenes by the transition-metal-catalyzed reaction of a intermediate alkylborane with a sterically hindered nitroxyl radical. ...
04/22/2008
7361771Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1-pyrrole-3-carboxylic acid phenylamide
An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight ...
04/22/2008
7358273Inhibitors of caspases
The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and...
04/15/2008
7358274Methods for treating or preventing cancer using Benzopyranone Compounds
This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyra...
04/15/2008
7348346Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
The present invention relates to compounds of formula (I), which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, sy...
03/25/2008
7329762Prodrugs of mitotic kinesin inhibitors
The present invention relates to phosphate ester prodrugs of dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relate...
02/12/2008
7319132Polymer compounds containing oxetane and maleimide functionality
Polymeric compounds containing an oxetane functionality and a maleimide functionality have the structure in which polymer is a polymeric backbone, m and n are integers from 2 to 500, R1 is methyl or et...
01/15/2008
7319130Phenolic resins
The invention herein disclosed comprises the use of oxazolidines, nitroalcohols, nitroamines, aminonitroalcohols, imines, hexahydropyimidines, nitrones, hydroxylamines, nitro-olefins and nitroacetals to serve as hardeners and/or as catalysts for curing phenolic resi...
01/15/2008
7319148Combinatorial production of nucleotide and nucleoside (XiTP) analogues
The invention concerns novel nucleotide analogues comprising a reactive hydrazide function used as initial synthons for preparing compounds (formula I) capable of inducing mutations or capable of inhibiting a DNA polymerase or a kinase. The invention also concerns n...
01/15/2008
7319131Phenolic resins
The invention herein disclosed comprises the use of oxazolidines, nitroalcohols, nitrones, halonitroparaffins, oxazines, azaadamantanes, hexamethylenetetramine salts, nitroamines, imidazolidines, triazines, nitrooxazolidines, and imidazolidine-oxazolidine hybrids to...
01/15/2008
7317063Phenolic resins
The invention herein disclosed comprises the use of oxazolidines, nitroalcohols, nitroamines, aminonitroalcohols, imines, hexahydropyrimidines, nitrones, hydroxylamines, nitro-olefins and nitroacetals to serve as hardeners and/or as catalysts for curing phenolic res...
01/08/2008
7317064Phenolic resin systems for fiber reinforced composite manufacture
The invention includes formulations useful for creating reinforced composites based on 1) novolac resin compositions, and, 2) non-formaldehyde hardeners, as well as processes for manufacturing components using said reinforced composites. ...
01/08/2008
7312336Compounds with analgesic effect
Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use ...
12/25/2007
73040871-acyl-pyrrolidine derivatives for the treatment of viral infections
Anti-viral agents of Formula (I) wherein: A represents hydroxy; D represents aryl or heteroaryl; E represents hydrogen, C1-6alkyl, aryl, heteroaryl or heterocyclyl; G represents hydrogen or o...
12/04/2007
7282510Small molecule inhibitors of rotamase enzyme activity
This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prol...
10/16/2007
7279471Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula wherein A and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydra...
10/09/2007
7276531G-lactam derivatives as prostaglandin agonists
A gamma-lactam diene of Formula I: which is particularly useful as a medicament for the treatment of various disorders such as asthma, hypertension, osteoporosis, sexual dysfunction and fertility disorders. ...
10/02/2007
7259179Kinase inhibitors
A compound of the general formula: or pharmaceutically acceptable salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating protein kinase-associated disease states usin...
08/21/2007
7250519Method for the production of arylamines
The invention relates to a method for the production of tertiary amines by reaction of secondary amines with aromatics or heteroaromatics in the presence of a base, a nickel or palladium compound and one or several phosphines, dialkoxy-, and/or diaryloxyphosphines i...
07/31/2007
7250414Diphenylmethyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined ...
07/31/2007
7238724Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
The present invention relates to compounds that inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and va...
07/03/2007
7232818Compounds for enzyme inhibition
Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited b...
06/19/2007
7232915Process for the synthesis of 1,3-diols
An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane spe...
06/19/2007
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